YH239-EE
- Product Name
- YH239-EE
- CAS No.
- 1364488-67-4
- Chemical Name
- YH239-EE
- Synonyms
- CS-1286;YH239-EE;YH239-EE USP/EP/BP;YH 239-EE;YH 239 EE;YH239-EE, 10 mM in DMSO;Ethyl 3-[2-(tert-Butylamino)-1-[N-(4-chlorobenzyl)formamido]-2-oxoet;Ethyl 3-(2-(tert-butylamino)-1-(N-(4-chlorobenzyl)formamido)-2-oxoethyl)-6-chloro-1H-indole-2-;Ethyl 3-(2-(tert-butylamino)-1-(N-(4-chlorobenzyl)formamido)-2-oxoethyl)-6-chloro-1H-indole-2-carboxylate;ethyl 3-[2-(tert-butylamino)-1-[(4-chlorophenyl)methyl-formylamino]-2-oxoethyl]-6-chloro-1H-indole-2-carboxylate;1H-Indole-2-carboxylic acid, 6-chloro-3-[1-[[(4-chlorophenyl)methyl]formylamino]-2-[(1,1-dimethylethyl)amino]-2-oxoethyl]-, ethyl ester
- CBNumber
- CB82710411
- Molecular Formula
- C25H27Cl2N3O4
- Formula Weight
- 504.41
- MOL File
- 1364488-67-4.mol
YH239-EE Property
- Boiling point:
- 763.3±60.0 °C(Predicted)
- Density
- 1.313±0.06 g/cm3(Predicted)
- storage temp.
- Desiccate at -20°C
- solubility
- ≥50.4 mg/mL in DMSO; insoluble in H2O; ≥4.26 mg/mL in EtOH with ultrasonic
- form
- solid
- pka
- 13.20±0.30(Predicted)
- color
- White to off-white
N-Bromosuccinimide Price
- Product number
- 27678
- Product name
- YH 239-EE
- Packaging
- 5mg
- Price
- $81
- Updated
- 2024/03/01
- Product number
- 27678
- Product name
- YH 239-EE
- Packaging
- 50mg
- Price
- $553
- Updated
- 2024/03/01
- Product number
- 27678
- Product name
- YH 239-EE
- Packaging
- 10mg
- Price
- $152
- Updated
- 2024/03/01
- Product number
- 27678
- Product name
- YH 239-EE
- Packaging
- 25mg
- Price
- $298
- Updated
- 2024/03/01
- Product number
- 6719
- Product name
- YH239-EE
- Purity
- ≥98%(HPLC)
- Packaging
- 50
- Price
- $513
- Updated
- 2021/12/16
YH239-EE Chemical Properties,Usage,Production
Uses
YH239-EE, the ethyl ester of YH239, is a potent p53-MDM2 antagonist and an apoptosis inducer.
Biological Activity
yh239-ee is a potent antagonist of p53-mdm2 [1].p53 is a transcription factor and functions as a tumor suppressor. mdm2 is a negative regulator of p53. the interaction of p53 and mdm2 has emerged as a novel target for anticancer drugs [1].yh239-ee is a potent p53-mdm2 antagonist. in oci-aml-3 cells, yh239-ee potently inhibited cell proliferation. in aml cell lines, yh239-ee induced a cell cycle arrest and cell accumulation in the sub-g1 phase. yh239-ee induced apoptosis by 11.8-fold, 5.6-fold and 13.1-fold in oci-aml-3, molm-13 and nb4 aml cell lines, respectively. in molm-13 cells, yh239 exhibited almost no apoptotic effect. however, yh239-ee significantly induced apoptosis. in molm-13 cells, (+)-yh239-ee and (−)-yh239-ee inhibited metabolic activity with ec50 values of 7.5 μm and 25.2 μm and induced apoptosis with 13.7% and 51.5% viable cells, respectively. (+)-yh239-ee (20 μm) induced p53 and significantly activated caspase 3 and 7 [1].
target
p53-MDM2
storage
Store at -20°C
References
[1]. huang y, wolf s, beck b, et al. discovery of highly potent p53-mdm2 antagonists and structural basis for anti-acute myeloid leukemia activities. acs chem biol, 2014, 9(3): 802-811.
YH239-EE Preparation Products And Raw materials
Raw materials
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